Affinity labeling is one of the powerful techniques for identification of the target proteins of drugs. Recently, we have developed a novel modular methodology for affinity labeling named MoAL. In this method, the three essential elements (ligand, labeling site, reactive site) of affinity probes are separated into individual module molecules: ligand module, labeling module, and reactive module. So, the method facilitates the design and synthesis of ligand module molecules with thus simplified structures.
Herein, we report a labeling study of cyclooxygenase (COX) by MoAL using ligand modules derived from anti-inflammatory drugs, which bind to COX to inhibit the production of prostaglandins. We successfully achieved the selective labeling of COX and the detection of endogenous COX from vesicular gland fraction.
